Allosteric interactions of staurosporine and other indolocarbazoles with N-[methyl-3H]scopolamine and acetylcholine at muscarinic receptor subtypes: Identification of a second allosteric site

Molecular Pharmacology

Volumn 58, Issue 1, 2000, Pages 194-206

  Lazareno, Sebastian ^a   Popham, Angela ^a   Birdsall, Nigel J M ^b  

^a MEDICAL RESEARCH COUNCIL   (United Kingdom)

^b NATIONAL INSTITUTE FOR MEDICAL RESEARCH   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

CARBAZOLE DERIVATIVE; CHOLINERGIC RECEPTOR; INDOLE DERIVATIVE; MUSCARINIC RECEPTOR; RECEPTOR SUBTYPE; SCOPOLAMINE; STAUROSPORINE;

ACETYLCHOLINE RELEASE; ALLOSTERISM; ANIMAL CELL; ARTICLE; BINDING AFFINITY; CELL INTERACTION; CHO CELL; COMPETITIVE INHIBITION; LIGAND BINDING; NONHUMAN; PRIORITY JOURNAL; PROTON NUCLEAR MAGNETIC RESONANCE; RECEPTOR AFFINITY; RECEPTOR BINDING; RECEPTOR POTENTIAL;

EID: 0033945117     PISSN: 0026895X     EISSN: None     Source Type: Journal    
DOI: 10.1124/mol.58.1.194     Document Type: Article

References (21)

1. Birdsall NJM, Farries T, Gharagozloo P, Kobayashi S, Kuonen D, Lazareno S, Popham A and Sugimoto M (1997) Selective allosteric enhancement of the binding and actions of acetylcholine at muscarinic receptor subtypes. Life Sci 60:1047-1052.
2. Buckley NJ, Bonner TI, Buckley CM and Brann MR (1989) Antagonist binding properties of five cloned muscarinic receptors expressed in CHO-K1 cells. Mol Pharmacol 35:469-476.
3. Christopoulos A, Lanzafame A and Mitchelson F (1998) Allosteric interactions at muscarinic cholinoceptors. Clin Exp Pharmacol Physiol 25:185-194.
4. Ehlert FJ (1988) Estimation of the affinities of allosteric ligands using radioligand binding and pharmacological null methods. Mol Pharmacol 33:187-194.
5. Ellis J (1997) Allosteric binding sites on muscarinic Receptors. Drug Dev Res 40: 193-204.
6. Ellis J and Seidenberg M (1992) Two allosteric modulators interact at a common site on cardiac muscarinic receptors. Mol Pharmacol 42:638-641.
7. Gnagey A and Ellis J (1996) Allosteric regulation of the binding of [3H]acetylcholine to M2 muscarinic receptors. Biochem Pharmacol 52:1767-1775.
8. Holzgrabe U and Mohr K (1998) Allosteric modulators of ligand binding to muscarinic acetylcholine receptors. Drug Discovery Today 3:214-222.
9. Jakubik J, Bacakova L, El-Fakahany EE and Tucek S (1997) Positive cooperativity of acetylcholine and other agonists with allosteric ligands on muscarinic acetylcholine receptors. Mol Pharmacol 52:172-179.
10. Kase H, Iwahashi K, Nakanishi S, Matsuda Y, Yamada K, Takahashi M, Murakata C, Sato A and Kaneko M (1987) K-252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases. Biochem Biophys Res Commun 142:436-440.
11. Kleinsehroth J, Hartenstein J, Rudolph C and Schachtele C (1995) Novel indolocarbazole protein kinase C inhibitors with improved biochemical and physicochemical properties. Bioorg Med Chem Lett 5:55-60.
12. Lazareno S and Birdsall NJM (1993) Estimation of competitive antagonist affinity from functional inhibition curves using the Gaddum, Schild and Cheng-Prusoff equations. Br J Pharmacol 109:1110-1119.
13. Lazareno S and Birdsall NJM (1995) Detection, quantitation, and verification of allosteric interactions of agents with labeled and unlabeled ligands at G protein-coupled receptors: Interactions of strychnine and acetylcholine at muscarinic receptors. Mol Pharmacol 48:362-378.
14. Lazareno S and Birdsall NJM (1999) Measurement of competitive and allosteric interactions in radioligand binding studies, in G-Protein-Coupled Receptors (Haga T and Berstein G eds) pp 1-48, CRC Press, Boca Raton, FL.
15. Lazareno S, Gharagozloo P, Kuonen D, Popham A and Birdsall NJM (1998) Subtype-selective positive cooperative interactions between brucine analogues and acetylcholine at muscarinic receptors: Radioligand binding studies. Mol Pharmacol 53:573-589.
16. 3 receptors by brucine and gallamine. Br J Pharmacol 126: 290P.
17. Potter LT, Ferrendelli CA, Hanchett HE, Hollifield MA and Lorenzi MV (1989) Tetrahydroaminoacridine and other allosteric antagonists of hippocampal M1 muscarine receptors. Mol Pharmacol 35:652-660.
18. ++-dependent protein kinase. Biochem Biophys Res Commun 136:397-402.
19. Tränkle C, Kostenis E, Burgmer U and Mohr K (1996) Search for lead structures to develop new allosteric modulators of muscarinic receptors. J Pharmacol Exp Ther 279:926-933.
20. Tränkle C and Mohr K (1997) Divergent modes of action among cationic allosteric modulators of muscarinic M2 receptors. Mol Pharmacol 51:674-682.
21. Waelbroeck M (1994) Identification of drugs competing with D-tubocurarine for an allosteric site on cardiac muscarinic receptors. Mol Pharmacol 46:685-692.